EP2144921A2 — Phosphate modified nucleosides useful as substrates for polymerases and as antiviral agents

USPTO Abstract

This invention provides phosphate-modified nucleosides represented by the structural formula: wherein - B is a pyrimidine or purine base, or an analogue thereof, optionally substituted with one or two substituents independently selected from the group consisting of halogen, hydroxyl, sulfhydryl, methyl, ethyl, amino and methylamino; - R1 is H or OH; - R3 is selected from the group consisting of H, C1-6 alkyl, C3-6 cycloalkyl, aryl-C1-6alkyl and 2-cyanoethyl, wherein said C1-6 alkyl, C3-6 cycloalkyl or aryl-C1-6 alkyl is optionally substituted with one or more, preferably 1, 2 or 3, substituents independently selected from the group consisting of halogen, OH, C1-6 alkoxy, trifluoromethyl, trifluoromethoxy, nitro, cyano and amino; - W is O or S; and - R2 is a group derived from an amino-acid. These compounds are useful as substrates for DNA/RNA polymerases, and as anti-viral agents.